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dc.contributor.authorNirthanan, Selvanayagamen_US
dc.contributor.authorGwee, Matthew C. E.en_US
dc.date.accessioned2017-04-24T13:02:56Z
dc.date.available2017-04-24T13:02:56Z
dc.date.issued2004en_US
dc.date.modified2009-09-28T06:52:29Z
dc.identifier.issn13478613en_US
dc.identifier.doi10.1254/jphs.94.1en_AU
dc.identifier.urihttp://hdl.handle.net/10072/25852
dc.description.abstractThe discovery, about forty years ago, of a-bungarotoxin, a three-finger a-neurotoxin from Bungarus multicinctus venom, enabled the isolation of the nicotinic acetylcholine receptor (nAChR), making it one of the most thoroughly characterized receptors today. Since then, the sites of interaction between a-neurotoxins and nAChRs have largely been delineated, revealing the remarkable plasticity of the three-finger toxin fold that has optimally evolved to utilize different combinations of functional groups to generate a panoply of target specificities to discern subtle differences between nAChR subtypes. New facets in toxinology have now broadened the scope for the use of a-neurotoxins in scientific discovery. For instance, the development of short, combinatorial library-derived, synthetic peptides that bind with sub-nanomolar affinity to a-bungarotoxin and prevent its interaction with muscle nAChRs has led to the in vivo neutralization of experimental a-bungarotoxin envenomation, while the successful introduction of pharmatopes bearing "a-bungarotoxin-sensitive sites" into toxin-insensitive nAChRs has permitted the use of various a-neurotoxin tags to localize and characterize new receptor subtypes. More ambitious strategies can now be envisaged for engineering rationally designed novel activities on three-finger toxin scaffolds to generate lead peptides of therapeutic value that target the nicotinic pharmacopoeia. This review details the progress made towards achieving this goal.en_US
dc.description.peerreviewedYesen_US
dc.description.publicationstatusYesen_AU
dc.languageEnglishen_US
dc.language.isoen_AU
dc.publisherJapanese Pharmacological Societyen_US
dc.publisher.placeJapanen_US
dc.relation.ispartofpagefrom1en_US
dc.relation.ispartofpageto17en_US
dc.relation.ispartofissue1en_US
dc.relation.ispartofjournalJournal of Pharmacological Sciencesen_US
dc.relation.ispartofvolume94en_US
dc.subject.fieldofresearchBasic Pharmacologyen_US
dc.subject.fieldofresearchToxicology (incl. Clinical Toxicology)en_US
dc.subject.fieldofresearchcode111501en_US
dc.subject.fieldofresearchcode111506en_US
dc.titleThree-Finger α-Neurotoxins and the Nicotinic Acetylcholine Receptor, Forty Years Onen_US
dc.typeJournal articleen_US
dc.type.descriptionC1 - Peer Reviewed (HERDC)en_US
dc.type.codeC - Journal Articlesen_US
gro.date.issued2004
gro.hasfulltextNo Full Text


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